Eye sterile suspension containing loteprednol etabonate and preparation method thereof

Abstract

The invention relates to an ophthalmic sterile suspension containing loteprednol etabonate, which contains 0.5 percent of loteprednol etabonate minicrystal particles and takes 0.3 percent to 0.8 percent of chlorobutanol as a preservative, 0.1 percent to 0.3 percent of tween-80 as a surface active agent, 0.1 percent to 0.5 percent of hydroxypropylmethyl cellulose as a suspending agent, 0.03 percent to 0.08 percent of natrium adetate as a metal ion complexing agent, and glycerin and sodium chloride as an osmotic pressure regulator. The ophthalmic sterile suspension is prepared by respectively adopting different sterilization methods to the loteprednol etabonate and other components. Apart from the components, the ophthalmic sterile suspension also contains 0.3 percent of tobramycin.

Description

technical field [0001] The invention relates to an ophthalmic sterile suspension containing loteprednol etabonate, which is prepared by adopting different sterilization methods for loteprednol etabonate and other ingredients. Background technique [0002] Loteprednol etabonate is a new type of corticosteroid carrier anti-inflammatory drug, the chemical name is 11β, 17-dihydroxy-3-oxoandrost-1,4-diene-17β-chloromethyl formate 17-(B After topical administration in the eyes, it quickly penetrates the cornea and enters the anterior chamber, and can be rapidly inactivated after entering the blood circulation, so that it retains the strong local anti-inflammatory effect of corticosteroids, but no other corticosteroids systemic toxicity of drugs. Loteprednol etabonate can bind to the glucocorticoid receptor in the eye, so it can easily penetrate the cornea. Its action strength is 1.5 times greater than that of dexamethasone. It has good local activity and a high therapeutic index....

AI Technical Summary

Problems solved by technology

[0004] Secondly, the sterilization process of the ophthalmic sterile suspension is very important to the quality and stability of the product, because loteprednol etabonate is insoluble in water, exists in the form of crystalline particles in the suspension, and cannot pass through the 0.22μm The bacteria-removing filter membrane, damp heat sterilization can affect its crystal form and stability, and the sterilization problem of loteprednol etabonate is not mentioned in the above-mentioned published patent

Images